Acetylfentanyl (acetyl fentanyl) is an
opioid
Opioids are substances that act on opioid receptors to produce morphine-like effects. Medically they are primarily used for pain relief, including anesthesia. Other medical uses include suppression of diarrhea, replacement therapy for opioi ...
analgesic
An analgesic drug, also called simply an analgesic (American English), analgaesic (British English), pain reliever, or painkiller, is any member of the group of drugs used to achieve relief from pain (that is, analgesia or pain management). It ...
drug that is an
analog
Analog or analogue may refer to:
Computing and electronics
* Analog signal, in which information is encoded in a continuous variable
** Analog device, an apparatus that operates on analog signals
*** Analog electronics, circuits which use analo ...
of
fentanyl
Fentanyl, also spelled fentanil, is a very potent synthetic opioid used as a pain medication. Together with other drugs, fentanyl is used for anesthesia. It is also used illicitly as a recreational drug, sometimes mixed with heroin, cocaine ...
. Studies have estimated acetylfentanyl to be fifteen times more potent than
morphine
Morphine is a strong opiate that is found naturally in opium, a dark brown resin in poppies ('' Papaver somniferum''). It is mainly used as a pain medication, and is also commonly used recreationally, or to make other illicit opioids. Ther ...
,
which would mean that despite being somewhat weaker than fentanyl, it is nevertheless still several times stronger than pure
heroin. It has never been licensed for medical use and instead has only been sold as a
designer drug
A designer drug is a structural or functional analog of a controlled substance that has been designed to mimic the pharmacological effects of the original drug, while avoiding classification as illegal and/or detection in standard drug tests. Des ...
. Acetylfentanyl was discovered at the same time as fentanyl itself and had only rarely been encountered on the illicit market in the late 1980s. However, in 2013, Canadian police seized 3 kilograms of acetylfentanyl. As a
μ-opioid receptor
The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...
agonist, acetylfentanyl may serve as a direct substitute for heroin or other opioids. Common side effects of
fentanyl
Fentanyl, also spelled fentanil, is a very potent synthetic opioid used as a pain medication. Together with other drugs, fentanyl is used for anesthesia. It is also used illicitly as a recreational drug, sometimes mixed with heroin, cocaine ...
analogs are similar to those of fentanyl itself, which include
itching
Itch (also known as pruritus) is a sensation that causes the desire or reflex to scratch. Itch has resisted many attempts to be classified as any one type of sensory experience. Itch has many similarities to pain, and while both are unpleasant ...
,
nausea
Nausea is a diffuse sensation of unease and discomfort, sometimes perceived as an urge to vomit. While not painful, it can be a debilitating symptom if prolonged and has been described as placing discomfort on the chest, abdomen, or back of the ...
and potentially serious
respiratory depression
Hypoventilation (also known as respiratory depression) occurs when ventilation is inadequate (''hypo'' meaning "below") to perform needed respiratory gas exchange. By definition it causes an increased concentration of carbon dioxide ( hypercapn ...
, which can be life-threatening. Fentanyl analogs have killed hundreds of people throughout Europe and the former Soviet republics since the most recent resurgence in use began in Estonia in the early 2000s, and novel derivatives continue to appear.
Deaths
Europe
Acetylfentanyl has been analytically confirmed in 32 fatalities in four European member states between 2013 and August 2015, Germany (2), Poland (1), Sweden (27) and the United Kingdom (2).
Russia
Twelve deaths have been associated with acetylfentanyl in Russia since 2012.
United States
The
Centers for Disease Control and Prevention
The Centers for Disease Control and Prevention (CDC) is the national public health agency of the United States. It is a United States federal agency, under the Department of Health and Human Services, and is headquartered in Atlanta, Georg ...
(CDC) issued a health alert to report that between March 2013 and May 2013, 14 overdose deaths related to injected acetylfentanyl had occurred among intravenous drug users (ages between 19 and 57 years) in Rhode Island. After confirming five overdoses in one county, including a fatality, Pennsylvania asked coroners and medical examiners across the state to screen for acetylfentanyl. As a result of this investigation, Pennsylvania confirmed at least one acetylfentanyl overdose death and attributed at least 50 fatalities to either fentanyl or acetylfentanyl during the first half of 2013. In July 2015, the DEA informed about 52 confirmed fatalities involving acetylfentanyl in the United States between 2013 and 2015.
Japan
One fatal poisoning caused by intravenous injection of a "bath salt" product containing acetylfentanyl and
4'-Methoxy-α-pyrrolidinopentiophenone (''aka'' 4-MeO-α-PVP, a
substituted cathinone) has been reported in 2016.
Legal status
Canada
As an analog of fentanyl, acetylfentanyl is a
Schedule I Schedule 1 may refer to:
* Schedule I Controlled Substances within the US Controlled Substances Act
* Schedule I Controlled Drugs and Substances within the Canadian Controlled Drugs and Substances Act
* Schedule I Psychotropic Substances within th ...
controlled drug.
China
As of October, 2015 acetylfentanyl is a controlled substance in China.
United States
Acetylfentanyl is a
Schedule I Schedule 1 may refer to:
* Schedule I Controlled Substances within the US Controlled Substances Act
* Schedule I Controlled Drugs and Substances within the Canadian Controlled Drugs and Substances Act
* Schedule I Psychotropic Substances within th ...
controlled substance as of May 2015.
Switzerland
Acetylfentanyl is illegal in Switzerland as of December 2015.
United Kingdom
Acetylfentanyl was made a class A drug as an analogue of fentanyl in 1986.
Overdose
Acetylfentanyl overdosage has been reported to closely resemble heroin overdosage clinically. Additionally, while
naloxone
Naloxone, sold under the brand names Narcan (4 mg) and Kloxxado (8 mg) among others, is a medication used to reverse or reduce the effects of opioids. It is commonly used to counter decreased breathing in opioid overdose. Effects begin withi ...
(Narcan) is effective in treating acetylfentanyl overdose, larger than normal doses of the antidote may be required.
Detection in body fluids
Acetylfentanyl may be quantitated in blood, plasma or urine by
liquid chromatography-mass spectrometry
A liquid is a nearly incompressible fluid that conforms to the shape of its container but retains a (nearly) constant volume independent of pressure. As such, it is one of the four fundamental states of matter (the others being solid, gas, ...
to confirm a diagnosis of poisoning in hospitalized patients or to provide evidence in a medicolegal death investigation. Postmortem peripheral blood acetylfentanyl concentrations have been in a range of 89–945 μg/L in victims of acute overdosage.
See also
*
3-Methylbutyrfentanyl
3-Methylbutyrfentanyl (3-MBF) is an opioid analgesic that is an analog of butyrfentanyl.
Side effects of fentanyl analogs are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, whi ...
*
3-Methylfentanyl
*
4-Fluorofentanyl
Parafluorofentanyl (4-fluorofentanyl, pFF) is an opioid analgesic analogue of fentanyl developed by Janssen Pharmaceutica in the 1960s.
4-Fluorofentanyl was sold briefly on the US black market in the early 1980s, before the introduction of the ...
*
α-Methylfentanyl
α-Methylfentanyl (or ''alpha''-Methylfentanyl) an opioid analgesic that is an analog of fentanyl. It is sometimes sold as "China White".
History
α-Methylfentanyl was discovered by a team at Janssen Pharmaceutica in the 1960s. In 1976, it beg ...
*
Butyrfentanyl
*
Furanylfentanyl
Furanylfentanyl (Fu-F) is an opioid analgesic that is an analog of fentanyl and has been sold as a designer drug. It has an ED50 value of 0.02 mg/kg in mice. This makes it approximately one fifth as potent as fentanyl.
Side effects
Side ...
*
Homofentanyl
*
List of fentanyl analogues
This is a list of fentanyl analogues (sometimes referred to as Fentalogs), including both compounds developed by pharmaceutical companies for legitimate medical use, and those which have been sold as designer drugs and reported to national drug co ...
References
Further reading
*
{{Opioidergics
General anesthetics
Synthetic opioids
Piperidines
Anilides
Acetamides
Mu-opioid receptor agonists
Janssen Pharmaceutica
Belgian inventions
Euphoriants
Fentanyl